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Poly(ADP-Ribose) Polymerase-1 Inhibitors Drug Discovery, Design, and Development as Anticancer Agents from Past to

Arwa AlGhamdi1, Hanine AlMubayedh1

  • 1College of Pharmacy, Imam Abdulrahman bin Faisal University, Dammam, Saudi Arabia.

Mini Reviews in Medicinal Chemistry
|September 30, 2021
PubMed

Insights

Poly(ADP-Ribose) Polymerase (PARP) inhibitors offer targeted cancer therapy, particularly for BRCA-mutated tumors. Research is ongoing to address challenges like drug resistance and toxicity for improved efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cancer treatments often cause severe toxicities due to low selectivity.
  • Targeting DNA repair mechanisms, such as Poly(ADP-Ribose) Polymerase (PARP) inhibition, offers a selective approach to cancer cell death.
  • PARP inhibitors (PARPi) are particularly effective in tumors with pre-existing Homologous-Repair (HR) defects, like BRCA mutations.

Purpose of the Study:

  • To review the therapeutic applications of PARP inhibitors (PARPi) in cancer treatment.
  • To discuss the evolution of PARPi drug design and development.
  • To examine current challenges and future directions in PARPi therapy.

Main Methods:

  • Literature review of PARP inhibitors in cancer treatment.
  • Analysis of historical and current PARPi drug development.
  • Examination of clinical trial data and research findings.

Main Results:

  • Poly(ADP-Ribose) Polymerase (PARP) inhibition is a promising strategy for targeted cancer therapy.
  • The first PARPi, Olaparib, was approved in 2014 for BRCA-mutated ovarian cancer.
  • Ongoing research aims to overcome issues such as drug resistance and toxic accumulation.

Conclusions:

  • PARP inhibitors represent a significant advancement in targeted cancer therapy.
  • Further research is crucial to optimize PARPi efficacy and patient selection.
  • Addressing challenges like resistance and toxicity will enhance the clinical utility of PARPi.
Keywords:
BRCACancerDNA repairPARP inhibitorsolaparibpoly(ADP-Ribose) polymerase (PARP)

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